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SAR125884 hydrochlorid (1116743-46-4(free base))

SAR125884 hydrochlorid (1116743-46-4(free base))
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Purity:95%
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SAR125884 hydrochlorid (1116743-46-4(free base))

Catalog No. T5677
SAR125844 is a potent and selective MET kinase inhibitor with a favorable preclinical toxicity profile,(IC50=4.2 nM).
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Pack SizePriceAvailabilityQuantity
1 mg$53In Stock
5 mg$92In Stock
10 mg$153In Stock
25 mg$331In Stock
50 mg$488In Stock
100 mg$693In Stock
200 mg$995In Stock
1 mL x 10 mM (in DMSO)$171In Stock
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Product Introduction

Bioactivity
Description
SAR125844 is a potent and selective MET kinase inhibitor with a favorable preclinical toxicity profile,(IC50=4.2 nM).
Targets&IC50
MET RTK:4.2 nM
In vitro
MKN-45, Hs 746T, and SNU-5 cells were seeded in poly d-lysine 96-well plates in complete medium. Plates were incubated with increasing SAR125844 concentrations for 1 hour, cell lysates were generated using standard procedures and pMETY1230/1234/1235 level evaluated. IC50 values were calculated using the software and a 4-parameter logistic model[1].
In vivo
SAR125844 inhibited autophosphorylation of AXL and cell proliferation of TPM–NTRK1-overexpressing KM12 cell line with IC50 values of 110 and 1,400 nmol/L, respectively, indicating a 30- and 500-fold selectivity index for AXL and NTRK1 in cell-based assays. The selectivity profile of SAR125844 was further confirmed in cell lines with a single-digit nanomolar antiproliferative activity in MET-addicted cell lines and a complete lack of impact in cells not addicted to the MET pathway. This is in contrast to ARQ197 that has equal antiproliferative activity on MET-addicted and MET-independent tumor cell lines[1].
Animal Research
The antitumor activity of SAR125844 was investigated after administration of SAR125844 solution daily in SNU-5 bearing mice at 10, 20, and 45 mg/kg and every 2 days in Hs 746T tumor–bearing mice (at 5, 10, 20, and 45 mg/kg for SAR125844 solution and at 5, 11, 21, 53, 106, and 213 mg/kg for SAR125844 nanosuspension). Tumor volumes (in mm^3, based on the following formula, volume = length (mm) × width2 (mm2)/2), were measured twice weekly and body weight recorded every day. Endpoints collected were complete regressions (CR, regression below the palpable limit), partial regressions (PR, regression of 50% of the initial tumor volume), and the percentage of tumor regression (% of volume decrease posttreatment compared with pretreatment). Statistical significance was determined by a Dunnett test versus vehicle after a two-way ANOVA with repeated measures performed separately on ranks of changes from baseline with P < 0.05 considered significant[1].
Chemical Properties
Molecular Weight587
FormulaC25H23FN8O2S2.HCl
Cas No.
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 55 mg/mL (93.7 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7036 mL8.5179 mL17.0358 mL85.1789 mL
5 mM0.3407 mL1.7036 mL3.4072 mL17.0358 mL
10 mM0.1704 mL0.8518 mL1.7036 mL8.5179 mL
20 mM0.0852 mL0.4259 mL0.8518 mL4.2589 mL
50 mM0.0341 mL0.1704 mL0.3407 mL1.7036 mL

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